Purdue Pharma L.p.

Euro-celtique S.a.

Neurovance, Inc.

Dov Pharmaceutical, Inc.

Aton Pharma, Inc.

Otsuka America Pharmaceutical, Inc.

Shionogi, Inc.

Euthymics Bioscience, Inc.

Zhengming Chen

Sam Victory

Donald Kyle

Phil Skolnick

R Richard Goehring

John Whitehead

Joseph William Epstein

Anthony Basile

Qun Sun

Laykea Tafesse

Jiangchao Yao

Kevin Halloran

Bin Shao

Parviz Gharagozloo

Khondaker Islam

Alex Comely

Shyam Krishnan

Xiaoming Zhou

Samuel F Victory

Deyou Sha

John W F Whitehead

Xiaoming Chen

Ji Yang

Elfrida R Benjamin

An ospemifene solid dispersion for enhancing solubility and bioavailability, and methods of preparation thereof are disclosed. The solid dispersion comprises an active pharmaceutical ingredient, such as ospemifene, and a hydfophilie carrier, such as copovidone, hypromellose acetate succinate, polyvinylpyrrolidine, a polyvinylpyrrolidine/vinyl acetate co-polymer, hydroxyl propyl methylcellulose, hypromellose acetate succinate, a Eudragit&#xae; compound, hydroxypropylcellulose, a polyvinyl caprolactam-polyvinyl acetate polyethylene glycol graft co-polymer, hydroxypropyl methylcellulose phthalate, and mixtures thereof, and optionally a surfactant The ospemifene solid, dispersions can be used in methods of treating a symptom related, to menopause, such as vaginal dryness or sexual dysfunction, or in methods of treating osteoporosis.

Solid dispersions

The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

1-aryl-3-azabicyclo[3.1.0]hexanes: preparation and use to treat neuropsychiatric disorders

The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.

1-heteroaryl-3-azabicyclo[3.1.0]hexanes, methods for their preparation and their use as medicaments

Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.

Stereoselective synthesis of metyrosine

The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R-Rand Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain. 

4-phenylsulfonamidopiperidines as calcium channel blockers

The invention relates to piperidinyl and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R-R, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain. 

Benzenesulfonamide compounds and their use as blockers of calcium channels

The invention relates to fused and spirocycle compounds of Formula I: 

Fused and spirocycle compounds and the use thereof

A compound of the formula (I), (II), (III) or (IV) 

Nociceptin analogs

The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R-Rand Z are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain. 

Benzenesulfonamide compounds and their use

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Belle Mead, NJ, United States of America

Zhengming Chen